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Bombesin/gastrin-releasing Peptide Antagonists RC-3095 and RC-3940-II Inhibit Tumor Growth and Decrease the Levels and mRNA Expression of Epidermal Growth Factor Receptors in H-69 Small Cell Lung Carcinoma

Bombesin/gastrin-releasing Peptide Antagonists RC-3095 and RC-3940-II Inhibit Tumor Growth and Decrease the Levels and mRNA Expression of Epidermal Growth Factor Receptors in H-69 Small Cell Lung Carcinoma

M Koppán, G Halmos, J M Arencibia, N Lamharzi, A V Schally

Cancer. 1998 Oct 1;83(7):1335-43.

PMID: 9762934

Abstract:

Background:
Antagonists of bombesin/gastrin-releasing peptide (BN/GRP) have been developed to block the autocrine stimulatory effect of BN/GRP on tumors such as small cell lung carcinoma (SCLC). Although several studies have addressed the intracellular events that follow the formation of the receptor-ligand complex, the mechanism of action of BN/GRP antagonists remains unclear.
Methods:
In this study the authors investigated the effect of synthetic BN/GRP antagonists RC-3095 and RC-3940-II on tumor growth and the expression of epidermal growth factor receptors (EGF-R) in H-69 SCLC. Athymic nude mice xenografted with H-69 SCLC were treated subcutaneously for 5 weeks with RC-3095 and RC-3940-II at the dose of 10 microg/animal/day.
Results:
RC-3095 decreased tumor volume by approximately 50% (P < 0.05) and RC-3940-II by 70-60% (P < 0.01). Tumor burden also was significantly decreased in the groups treated with RC-3095 and RC-3940-II. Receptor analyses demonstrated high affinity binding sites for BN/GRP and EGF on the untreated H-69 SCLC tumors. After treatment with RC-3095 and RC-3940-II, the concentration of receptors for BN/GRP was decreased by 29.0% and 36.5%, respectively (both, P < 0.01) compared with controls, and EGF-R levels were reduced by 62.3% and 63.0%, respectively (both, P < 0.01). Reverse transcriptase-polymerase chain reaction and Southern blot analyses revealed that the levels of mRNA for EGF-R in tumors were lowered by 31% (P < 0.05) and 43% (P < 0.01), respectively, after treatment with RC-3095 and RC-3940-II.
Conclusions:
This study indicates that the inhibition of growth of H-69 SCLC by BN/GRP antagonists RC-3095 and RC-3940-II is accompanied by a marked decrease in the levels and mRNA expression of EGF-R.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP138147781	RC-3095		138147-78-1	Price

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